Assay Detail
Functional
CHEMBL771384
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Blockade of calcium-evoked contractions in depolarized aortic strips
16
Total Activities
16
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Functional |
| Organism | Oryctolagus cuniculus |
| Tissue | Aorta |
| Confidence | 9 — Direct single protein target |
| Curated By | Expert |
Target
Voltage-dependent L-type calcium channel subunit alpha-1C (CHEMBL2830) ↗| Type | SINGLE PROTEIN |
| Organism | Oryctolagus cuniculus |
Publication
Synthesis of 3-[(2,3-dihydro-1,1,3-trioxo-1,2-benzisothiazol-2-yl)alkyl] 1,4-dihydropyridine-3,5-dicarboxylate derivatives as calcium channel modulators.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 16 | 8.04 | 8.85 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL78656 | — | — | 1 | 8.85 |
| CHEMBL78651 | — | — | 1 | 8.54 |
| CHEMBL193 | NIFEDIPINE | 4.0 | 1 | 8.54 |
| CHEMBL81326 | — | — | 1 | 8.48 |
| CHEMBL312276 | — | — | 1 | 8.44 |
| CHEMBL80771 | — | — | 1 | 8.29 |
| CHEMBL432933 | — | — | 1 | 8.29 |
| CHEMBL312103 | — | — | 1 | 8.11 |
| CHEMBL79740 | — | — | 1 | 8.00 |
| CHEMBL311556 | — | — | 1 | 7.88 |
| CHEMBL78790 | — | — | 1 | 7.82 |
| CHEMBL78944 | — | — | 1 | 7.60 |
| CHEMBL80501 | — | — | 1 | 7.60 |
| CHEMBL77615 | — | — | 1 | 7.51 |
| CHEMBL433325 | — | — | 1 | 7.42 |
| CHEMBL78396 | — | — | 1 | 7.19 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL78656 | — | IC50 | = | 1.4 | nM | 8.85 |
| CHEMBL78651 | — | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL193 | NIFEDIPINE | IC50 | = | 2.9 | nM | 8.54 |
| CHEMBL81326 | — | IC50 | = | 3.3 | nM | 8.48 |
| CHEMBL312276 | — | IC50 | = | 3.6 | nM | 8.44 |
| CHEMBL80771 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL432933 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL312103 | — | IC50 | = | 7.8 | nM | 8.11 |
| CHEMBL79740 | — | IC50 | = | 10.1 | nM | 8.00 |
| CHEMBL311556 | — | IC50 | = | 13.3 | nM | 7.88 |
| CHEMBL78790 | — | IC50 | = | 15.1 | nM | 7.82 |
| CHEMBL78944 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL80501 | — | IC50 | = | 25.1 | nM | 7.60 |
| CHEMBL77615 | — | IC50 | = | 30.9 | nM | 7.51 |
| CHEMBL433325 | — | IC50 | = | 38.0 | nM | 7.42 |
| CHEMBL78396 | — | IC50 | = | 64.5 | nM | 7.19 |